Phase Behavior of Doxycycline Hyclate-Incorporated Bleached Shellac In Situ Forming Gel/Microparticle after Solvent Movement

2020 ◽  
Vol 859 ◽  
pp. 21-26
Author(s):  
Setthapong Senarat ◽  
Juree Charoenteeraboon ◽  
Pitsiree Praphanwittaya ◽  
Thawatchai Phaechamud

With regard to the periodontal pocket application of in situ forming systems, the understanding the phase behavior after solidification owing to solvent movement could verify the deformability of specimen and its capacity to reside in the artificial periodontal pocket. The aim of this research was to investigate the phase behavior by determining mechanical properties as hardness and elasticity/plasticity ratio with texture analyzer for matrices obtained from drug-free and doxycycline hyclate (DX)-incorporated bleached shellac (BS) in situ forming gel (isg) and –microparticle (ism) after solvent exchange. The solvents for dissolving BS were 2-pyrrolidone (PYR), N-methyl pyrrolidone (NMP) and dimethyl sulfoxide (DMSO). The matrix from isg was less rough and bulge than that of isg. The order of mechanical hardness of transformed system prepared with different solvents was presented as PYR > NMP > DMSO, influenced by phase separation rate and porosity. The systems prepared with NMP and DMSO were more likely plastic or able to adapt its geometry to dynamic changes while that prepared with PYR was elastic. DX-incorporated ism matrix was still governed by the oil in external phase; thus, its consequence was reasonably plastic instead. XRD pattern indicated that the solvent type had no effect on the crystallinity of remained BS after solvent movement. SEM topography revealed sponge-like structure of isg prepared with DMSO and NMP whereas that prepared with PYR exhibited only initiated diminutive pores. The size and density of pores increased by time of isg using different solvents as following DMSO > NMP > PYR, whereas ism matrices had less pore density. The level of porosity of each matrix reflected the mechanical strength that a higher porous structure collapsed easily but a dense matrix considerably resisted to a compression.

2015 ◽  
Vol 659 ◽  
pp. 8-12
Author(s):  
Pitsiree Praphanwittaya ◽  
Thawatchai Phaechamud

Bleached shellac (BS), a biodegradable natural resin purified from insect lac, has been used in a varity of controlled drug delivery systems. Nevertheless, there were negligible researches explored the potential of it as in injectable in situ microparticles (ISM) applications. The goal of this study was to utilize BS to form ISM (shellac-solution dispersed into an external olive oil phase, as o/o emulsion) prepared by two-syringe technique. Addition of glyceryl monostearate (GMS) as stabilizer obviously decreased the emulsion droplet size. ISM emulsion comprising 5% w/w GMS in external phase could form into droplets and precipitate in form of microparticles after exposure to phosphate buffer. 2-Pyrrolidone was the most appropriate solvent to form massive microparticles with regular shape especially at ratio of 7:3 external:internal phases. ISM transformation was occurred after exposure to phosphate buffer and tended to reduce the droplet size when ratio of external phase was higher than 50%. Incorporation of doxycycline hyclate did not influence the amount and size of ISM. Therefore shellac exhibited as an alternative polymer matrix for ISM which higher amount of GMS could reduce the size of emulsion droplet and volume phase ratio seriously influenced on emulsion size and ISM formation.


2020 ◽  
Vol 859 ◽  
pp. 120-124
Author(s):  
Sarun Tuntarawongsa ◽  
Jongjan Mahadlek ◽  
Nutdanai Lertsuphotvanit ◽  
Thawatchai Phaechamud

The release behavior of doxycycline hyclate (DH) from beta-cyclodextrin (β-CD) in situ gels (ISG) and in situ microparticles (ISM) was investigated using dialysis tube method and direct contact method compared to that from DH solution. From dialysis tube method, DH released completely from solution within 8 h, while it released with more sustainable from ISM and ISG completely at 12 h and 28 h, respectively. The release pattern of them was similar when tested using direct contact method (released completely at 9 days). The DH release from dialysis tube method of all systems was a first order kinetic. DH release from ISM using direct contact method fitted well with a Higuchi’s equation. The dialysis tube method was suitable for determining formula factors affecting the drug release behavior. However, to simulate the pocket condition with contact area is limited, the drug release test with direct contact method was preferred than dialysis tube method.


2019 ◽  
Vol 819 ◽  
pp. 221-226 ◽  
Author(s):  
Nutdanai Lertsuphotvanit ◽  
Pornsit Chaiya ◽  
Thawatchai Phaechamud

In situ forming microparticle (ISM) is an injectable emulsion drug delivery system comprising drug loaded in polymeric solution as internal phase and oil combined with emulsifier as external phase. This emulsion transforms into microparticle after contact an aqueous environment by solvent exchange mechanism. This study developed ISM using internal phase comprising 5% w/w doxycycline hyclate (DH) loaded with various concentrations of beta-cyclodextrin (β-CD) using N-methyl-2-pyrrolidone (NMP) as a solvent and external phase containing olive oil combined with glyceryl monostearate (GMS). High concentrated β-CD solutions in NMP are used as the internal phase of ISM. Matrix forming behavior is evaluated for their particle size, transformation to microparticle, pH, rate of matrix formation, contact angle and surface tension. Each emulsion had similar pH values about 3.5-4.1 and transformed into microparticles (particle size about 60 μm) after contact with phosphate buffer pH 6.8. The particle sizes of each preparation decreased significantly after transformed into microparticles and the more microparticles were evident with time. The rate of matrix formation of ISM was apparent slower than its internal phase and was slower with time. Contact angle of ISM and its internal phase showed good wetting which the surface tension of 35% w/w β-CD ISM was 44.19 mN/m. The β-CD ISM exhibited as the potential delivery system for incorporation of active compounds.


2015 ◽  
Vol 659 ◽  
pp. 13-18 ◽  
Author(s):  
Jongjan Mahadlek ◽  
Thawatchai Phaechamud

In situforming gel with solvent exchange mechanism is one of drug delivery systems for periodontitis treatment. The system is injected into the desired site then transforms into a gel state when the solvent diffuses out and aqueous diffuses in. Thein situforming Eudragit RSgels loading 1, 5 and 10%w/w metronidazole (MT) were developed in this study usingN-methyl pyrrolidone (NMP), 2-pyrrolidone and dimethyl sulfoxide (DMSO) as solvent. The viscosity of the gel systems in all solvents were increased as drug or polymer amount was increased with Newtonian flow behavior. Transformation into gel was evident after initiated the systems in phosphate buffer pH 6.8. NMP systems exhibited the lowest work of syringeability through 18 G syringe. Drug release from dialysis tube of DMSO systems was slower than that of NMP and 2-pyrrolidone systems, respectively. Antimicrobial activity againstStaphylococcus aureusof the systems comprising MT using NMP as solvent was greater than that using 2-pyrrolidone and DMSO, respectively, which the antimicrobial activity was increased as the drug amount was increased. Therefore, the solvent type affected the viscosity, gel formation, syringeability, drug release and antimicrobial activity of Eudragit RS systems. These developed systems sustained the drug release and inhibited the bacterial growth hence they were interesting systems for periodontitis treatment.


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